摘要:

AbstractThis paper is an autobiographical study of the author's early work on the chemical cross‐linking of proteins as well as on oligomer and peptide synthesis from 1949 in Heidelberg until the synthesis of insulin in 1963 in Aachen.2Editor's note: Professor Zahn was born in 1916 in Erlangen and studied chemistry at, and graduated from, the University of Technology in Karlsruhe (Dr. Ing. in 1940). From 1940 to 1949 he was assistant to Professor Elöd at the Institute for Textile Chemistry in Karlsruhe and later in Badenweiler, and from 1949 to 1957 he was assistant to Professor Freudenberg at the Institute for Chemistry of the University of Heidelberg. From 1952 to 1985 he was Director of the German Wool Research Institute, and in 1960 was appointed full Professor at the University of Technology in Aachen.Copyright © 2000 European Peptide Society and John Wiley& Sons,

ISSN:1075-2617    

DOI:10.1002/(SICI)1099-1387(200001)6:1<1::AID-PSC238>3.0.CO;2-P

出版商:John Wiley&Sons, Ltd.    

年代:2000

数据来源: WILEY

摘要:

AbstractThe solid phase synthesis of a set of peptide aldehydes derived from the NS5A/NS5B junction of hepatitis C virus (HCV) viral polyprotein is demonstrated using an oxazolidine linker and the Multipin™ method. Deletion of the P6 and P5 residues results in a dramatic loss of inhibitory activity. Copyright © 2000 European Peptide Society and John Wiley&Sons, L

ISSN:1075-2617    

DOI:10.1002/(SICI)1099-1387(200001)6:1<11::AID-PSC229>3.0.CO;2-#

出版商:John Wiley&Sons, Ltd.    

年代:2000

数据来源: WILEY

摘要:

AbstractThe 32‐residue peptide, RK‐1, a novel kidney‐derived three disulfide‐bonded member of the antimicrobial α‐defensin family, was synthesized by the continuous flow Fmoc‐solid phase method. The crude, cleaved andS‐reduced linear peptide was both efficiently folded and oxidized in an acidic solution of aqueous dimethyl sulfoxide. Following purification of the resulting product, it was shown by a variety of analytical techniques, including matrix assisted laser desorption time of flight mass spectrometry, to possess a very high degree of purity. The disulfide bond pairing of the synthetic peptide was determined by1H‐NMR spectroscopy and confirmed to be a Cys1‐Cys6, Cys2‐Cys4, Cys3‐Cys5arrangement similar to other mammalian α‐defensin peptides. The synthetic RK‐1 was also shown to inhibit the growth ofEscherichia colitype strain NCTC 10418. Copyright © 2000 European Peptide Soci

ISSN:1075-2617    

DOI:10.1002/(SICI)1099-1387(200001)6:1<19::AID-PSC230>3.0.CO;2-1

出版商:John Wiley&Sons, Ltd.    

年代:2000

数据来源: WILEY

摘要:

AbstractA sandostatin analog, TT‐232 (D‐Phe‐c[Cys‐Tyr‐D‐Trp‐Lys‐Cys]‐Thr‐NH2), exhibits strong anti‐tumor effects bothin vitroandin vivo. In order to study the structure–activity relationships of TT‐232, we designed and synthesized an analog of TT‐232, namely Lan‐7, in which the disulfide bridge is replaced by a lanthionine monosulfide bridge. Conformational analysis by NMR spectroscopy and computer simulations revealed that Lan‐7 and TT‐232 adopt very similar conformations in solution, which are quite different from the preferred conformations of sandostatin. Lan‐7 has significant growth inhibition effects on a number of human tumor cell lines. It can also induce apoptosis in human ovarian carcinoma 2008 cells. At the same time, Lan‐7 produced no toxicity to normal human hematopoietic progenitor cells. All of these results indicate that the modification we made does not alter the anti‐tumor activity of TT‐232. Copyright © 2000 Europea

ISSN:1075-2617    

DOI:10.1002/(SICI)1099-1387(200001)6:1<26::AID-PSC231>3.0.CO;2-6

出版商:John Wiley&Sons, Ltd.    

年代:2000

数据来源: WILEY

摘要:

AbstractBased on the peculiar spatial array of the active sites in the internal chamber of the multicatalytic proteasome, as derived from the X‐ray structure of yeast proteasome, homo‐ and heterobivalent inhibitors were designed and synthesized to exploit the principle of multivalency for enhancing inhibition potency. Peptidic bis‐aldehyde compounds of the octapeptide size were synthesized to address adjacent active sites, whilst a PEG spacer with a statistical length distribution of 19–25 monomers was used to link two identical or different tripeptide aldehydes as binding heads. These bis‐aldehyde compounds were synthesized applying both methods in solution and solid phase peptide synthesis. Bivalent binding was observed only for the PEG‐spaced inhibitors suggesting that binding from the primed side prevents hemiacetal formation with the active site threonine residue. Copyright © 2000 European Peptide Society and John Wil

ISSN:1075-2617    

DOI:10.1002/(SICI)1099-1387(200001)6:1<36::AID-PSC232>3.0.CO;2-2

出版商:John Wiley&Sons, Ltd.    

年代:2000

数据来源: WILEY